Results 281 to 290 of about 31,985 (308)
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Heterocyclic fused pyridone carboxylic acid M1 positive allosteric modulators
Bioorganic & Medicinal Chemistry Letters, 2010The phenyl ring in a series of quinolone carboxylic acid M(1) positive allosteric modulators was replaced with a variety of heterocycles in order to reduce protein plasma binding and enhance CNS exposure.
Scott D, Kuduk +10 more
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Enantiospecific Positive Allosteric Modulation of α4β2 Nicotinic Receptor Subtypes
ACS Chemical NeuroscienceNicotinic acetylcholine receptors (nAChRs) are integral to brain function, playing critical roles in cognition and reward pathways. Among these, α4β2 nAChRs are key targets for developing therapeutics to address nicotine addiction and cognitive disorders.
Josue Gaona +9 more
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Benzoxazinones as potent positive allosteric AMPA receptor modulators: Part I
Bioorganic & Medicinal Chemistry Letters, 2011AMPA receptors (AMPARs) are an increasingly important therapeutic target in the CNS. Aniracetam, the first identified potentiator of AMPARs, led to the rigid and more potent CX614. This lead molecule was optimized in order to increase affinity towards the AMPA receptor.
Rudolf, Mueller +9 more
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Fused thiazolyl alkynes as potent mGlu5 receptor positive allosteric modulators
Bioorganic & Medicinal Chemistry Letters, 2013A new series of potent fused thiazole mGlu5 receptor positive allosteric modulators (PAMs) (10, 11 and 27-31) are disclosed and details of the SAR and optimization are described. Optimization of alkynyl thiazole 9 (Lu AF11205) led to the identification of potent fused thiazole analogs 10b, 27a, 28j and 31d.
Mathivanan, Packiarajan +8 more
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N-Aryl pyrrolidinonyl oxadiazoles as potent mGluR5 positive allosteric modulators
Bioorganic & Medicinal Chemistry Letters, 2012A novel series of N-aryl pyrrolidinonyl oxadiazoles were identified as mGluR5 positive allosteric modulators (PAMs). Optimization of the initial lead compound 6a led to the identification of the 12c (-) enantiomer as a potent compound with acceptable in vitro clearance, CYP, hERG and PK properties. Para substituted N-aryl pyrrolidinonyl oxadiazoles are
Mathivanan, Packiarajan +7 more
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mGluR5 positive allosteric modulators
Drugs of the Future, 2008null Chen, Y., null Conn, P.J.
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Positive allosteric modulators of the calcium-sensing receptor
2021The present invention relates to non-naturally occurring antibodies or active antibody fragments specifically binding the calcium-sensing receptor (CaSR), acting as positive allosteric modulators (PAMs) to provide for potent therapeutic agents. More particular, the immunoglobulin single variable domains (ISVDs) identified herein reveal a novel ...
Steyaert, Jan +6 more
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The gut microbiome as a modulator of healthy ageing
Nature Reviews Gastroenterology and Hepatology, 2022Tarini S Ghosh +2 more
exaly
AMPA Receptor Positive Allosteric Modulators – a Case History
2014Significant advances have been made over recent years in our understanding of the tremendous complexity underlying the function of the human brain, in particular gaining insight into the mechanisms of synaptic plasticity which are key to developmental, adaptive and learning processes.
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